CN113939518A - 作为激酶抑制剂的稠合三环化合物 - Google Patents

作为激酶抑制剂的稠合三环化合物 Download PDF

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Publication number
CN113939518A
CN113939518A CN202080020962.7A CN202080020962A CN113939518A CN 113939518 A CN113939518 A CN 113939518A CN 202080020962 A CN202080020962 A CN 202080020962A CN 113939518 A CN113939518 A CN 113939518A
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China
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compound
radical
formula
group
mmol
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CN202080020962.7A
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English (en)
Inventor
张汉承
程鑫
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Hangzhou Innogate Pharma Co Ltd
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Hangzhou Innogate Pharma Co Ltd
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Publication of CN113939518A publication Critical patent/CN113939518A/zh
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

一类含有三环杂芳基化合物。具体地,提供了如下式(I)所示结构的化合物、含有式(I)化合物的药物组合物及所述化合物,以及这些化合物的同位素衍生物,手性异构体,变构体,不同的盐,前药,制剂等等。式(I)化合物能够有效抑制蛋白激酶(包括EGFR、EGFR(C797S)、ALK、和HPK1等),从而起到治疗各种肿瘤的作用。

Description

PCT国内申请,说明书已公开。

Claims (1)

  1. PCT国内申请,权利要求书已公开。
CN202080020962.7A 2019-03-15 2020-03-16 作为激酶抑制剂的稠合三环化合物 Pending CN113939518A (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
CN201910199527 2019-03-15
CN2019101995274 2019-03-15
CN2019105444177 2019-06-21
CN201910544417 2019-06-21
CN202010023799 2020-01-09
CN2020100237991 2020-01-09
PCT/IB2020/052388 WO2020188467A1 (zh) 2019-03-15 2020-03-16 作为激酶抑制剂的稠合三环化合物

Publications (1)

Publication Number Publication Date
CN113939518A true CN113939518A (zh) 2022-01-14

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CN202080020962.7A Pending CN113939518A (zh) 2019-03-15 2020-03-16 作为激酶抑制剂的稠合三环化合物

Country Status (3)

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US (1) US20220153766A1 (zh)
CN (1) CN113939518A (zh)
WO (1) WO2020188467A1 (zh)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LT3873903T (lt) 2018-10-31 2024-05-10 Gilead Sciences, Inc. Pakeistieji 6-azabenzimidazolo junginiai, kaip hpk1 inhibitoriai
JP7273172B2 (ja) 2018-10-31 2023-05-12 ギリアード サイエンシーズ, インコーポレイテッド Hpk1阻害活性を有する置換6-アザベンゾイミダゾール化合物
EP3972695A1 (en) 2019-05-23 2022-03-30 Gilead Sciences, Inc. Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors
WO2022100688A1 (zh) * 2020-11-13 2022-05-19 南京红云生物科技有限公司 Hpk1激酶调节剂、其制备方法与应用
KR20220090443A (ko) * 2020-12-21 2022-06-29 주식회사 비투에스바이오 헤테로아릴 유도체 화합물 및 이의 용도
CN116848103A (zh) * 2021-04-08 2023-10-03 杭州阿诺生物医药科技有限公司 高活性hpk1激酶抑制剂
CN117865993B (zh) * 2023-01-10 2024-09-27 杭州师范大学 一种aak1抑制剂及其制备和应用

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102105150A (zh) * 2008-05-21 2011-06-22 阿里亚德医药股份有限公司 用作激酶抑制剂的磷衍生物
WO2017086829A1 (ru) * 2015-11-19 2017-05-26 Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") Дихлорацетаты замещенных n4-[2-(диметилфосфиноил) фенил]-n2-(2-метокси-4-пиперидин-1-илфенил)-5-хлорпиримидин-2,4-диаминов в качестве модуляторов alk и egfr, предназначенных для лечения рака
WO2017118438A1 (zh) * 2016-01-08 2017-07-13 杭州英创医药科技有限公司 作为fgfr抑制剂的杂环化合物
WO2018108084A1 (zh) * 2016-12-12 2018-06-21 杭州英创医药科技有限公司 一类含有三环杂芳基的化合物

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102105150A (zh) * 2008-05-21 2011-06-22 阿里亚德医药股份有限公司 用作激酶抑制剂的磷衍生物
WO2017086829A1 (ru) * 2015-11-19 2017-05-26 Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") Дихлорацетаты замещенных n4-[2-(диметилфосфиноил) фенил]-n2-(2-метокси-4-пиперидин-1-илфенил)-5-хлорпиримидин-2,4-диаминов в качестве модуляторов alk и egfr, предназначенных для лечения рака
WO2017118438A1 (zh) * 2016-01-08 2017-07-13 杭州英创医药科技有限公司 作为fgfr抑制剂的杂环化合物
WO2018108084A1 (zh) * 2016-12-12 2018-06-21 杭州英创医药科技有限公司 一类含有三环杂芳基的化合物

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WO2020188467A1 (zh) 2020-09-24
US20220153766A1 (en) 2022-05-19

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